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    • 12. 发明专利
    • BR0003105A
    • 2001-03-13
    • BR0003105
    • 2000-07-24
    • ADIR
    • GOLDSTEIN SOLOBOUTIN JEANPOISSONNET GUILLAUMEPARMENTIER JEAN-GILLESBRION JEAN-DANIELMILLAN MARKDEKEYNE ANNE
    • A61K31/437A61P1/00A61P15/00A61P25/00A61P25/06A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28C07B61/00C07D471/04A61K31/4375
    • 1-( beta -Carbolin-1-yl)-cycloalkanecarboxylic acid derivatives (I) are new. beta -Carboline derivatives of formula (I), and their isomers and acid or base addition salts, are new. dotted lines = optional bonds; R1 = H, alkyl, -R6-Q, -COOR7, -COR8 or -CONHR8; or is absent if the N of NR1 carries an intracyclic double bond; R6 = 1-6C alkylene; Q = cycloalkyl, aryl or heterocyclyl; R7 = alkyl, Q or -R6-Q; R8 = H or as R7; R2 = CN, COOR8, CONHR8, mono- or dialkylaminoalkylaminocarbonyl, NR8R9, NHCOOR7 or COR6; R9 = as R8; R3 + R4 = group completing 3-10C cycloalkyl; R5 = H, alkyl or arylalkyl; Ra-Rd = H, halo, alkyl, OH, alkoxy, trihaloalkyl, trihaloalkoxy, NO2, CN, NH2, mono- or dialkylamino, aryl, arylalkyl, alkoxycarbonyl, 1-6C acyl, aryloxy or arylalkoxy; cycloalkyl moiety = 3-10C mono- or bicyclic, saturated or mono- or polyunsaturated (but not aromatic) group (optionally substituted by one or more of halo, OH, alkyl and alkoxy); aryl moiety = phenyl, naphthyl, tetrahydronaphthyl, dihydronaphthyl, indenyl or indanyl group (optionally substituted by one or more of halo, OH, CN, NO2, alkyl, alkoxy, NH2, mono- or dialkylamino, aryloxy, arylalkoxy, trihaloalkyl, 1-6C acyl, alkoxycarbonyl, alkylaminocarbonyl and oxo); heterocyclyl moiety = 5-12 membered mono- or bicyclic, saturated or unsaturated, aromatic or non-aromatic group containing 1-3 of N, O and S as heteroatom(s) (optionally substituted by one or more of halo, OH, alkyl, alkoxy, NO2, oxo, NH2, and mono- or dialkylamino); alkyl moieties have 1-6C. An Independent claim is included for the preparation of (I).
    • 13. 发明专利
    • NO20003764D0
    • 2000-07-21
    • NO20003764
    • 2000-07-21
    • ADIR
    • GOLDSTEIN SOLOPOISSONNET GUILLAUMEPARMENTIER JEAN-GILLESBRION JEAN-DANIELMILLAN MARKDEKEYNE ANNEBOUTIN JEAN
    • A61K31/437A61P1/00A61P15/00A61P25/00A61P25/06A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28C07B61/00C07D471/04C07D
    • 1-( beta -Carbolin-1-yl)-cycloalkanecarboxylic acid derivatives (I) are new. beta -Carboline derivatives of formula (I), and their isomers and acid or base addition salts, are new. dotted lines = optional bonds; R1 = H, alkyl, -R6-Q, -COOR7, -COR8 or -CONHR8; or is absent if the N of NR1 carries an intracyclic double bond; R6 = 1-6C alkylene; Q = cycloalkyl, aryl or heterocyclyl; R7 = alkyl, Q or -R6-Q; R8 = H or as R7; R2 = CN, COOR8, CONHR8, mono- or dialkylaminoalkylaminocarbonyl, NR8R9, NHCOOR7 or COR6; R9 = as R8; R3 + R4 = group completing 3-10C cycloalkyl; R5 = H, alkyl or arylalkyl; Ra-Rd = H, halo, alkyl, OH, alkoxy, trihaloalkyl, trihaloalkoxy, NO2, CN, NH2, mono- or dialkylamino, aryl, arylalkyl, alkoxycarbonyl, 1-6C acyl, aryloxy or arylalkoxy; cycloalkyl moiety = 3-10C mono- or bicyclic, saturated or mono- or polyunsaturated (but not aromatic) group (optionally substituted by one or more of halo, OH, alkyl and alkoxy); aryl moiety = phenyl, naphthyl, tetrahydronaphthyl, dihydronaphthyl, indenyl or indanyl group (optionally substituted by one or more of halo, OH, CN, NO2, alkyl, alkoxy, NH2, mono- or dialkylamino, aryloxy, arylalkoxy, trihaloalkyl, 1-6C acyl, alkoxycarbonyl, alkylaminocarbonyl and oxo); heterocyclyl moiety = 5-12 membered mono- or bicyclic, saturated or unsaturated, aromatic or non-aromatic group containing 1-3 of N, O and S as heteroatom(s) (optionally substituted by one or more of halo, OH, alkyl, alkoxy, NO2, oxo, NH2, and mono- or dialkylamino); alkyl moieties have 1-6C. An Independent claim is included for the preparation of (I).